343307-74-4Relevant academic research and scientific papers
Synthesis and molecular modeling studies of indole-based antitumor agents
George, Riham F.,Panda, Siva S.,Shalaby, El-Sayed M.,Srour, Aladdin M.,Farag, I. S. Ahmed,Girgis, Adel S.
, p. 45434 - 45451 (2016)
Indole-based compounds 30-63 were synthesized by the multi-component 1,3-dipolar cycloaddition reaction of 1-alkyl-3,5-bis(arylidene)-4-piperidones 11-25 with azomethine ylides (generated by the condensation of isatins 26-28 with sarcosine 29). The single crystal X-ray studies of 46 and 48 supported the regio- and stereoselectivity of the reaction. Most of the synthesized spiro-indoles exhibited potent antitumor properties against the HeLa (cervical cancer) cell line through in vitro sulfo-rhodamine-B bioassay, higher than that of cisplatin. Only compound 54 showed bio-potency against the HepG2 (hepatocellular cancer) cell line, comparable to that of doxorubicin hydrochloride (standard reference). 3D-Pharmacophore and 2D-QSAR studies were used to validate the observed biological data and determine the most important parameters controlling activity. The estimated bio-properties from the computational studies showed high approximations to the experimental data.
CURCUMIN ANALOGS AND METHODS OF MAKING AND USING THEREOF
-
Page/Page column 65; 73; 74, (2014/02/16)
Compounds having Formula I or II, and methods of making and using thereof, are described herein:
